Preparation and Characterization of Solid Dispersion Telmisartan – Hydroxypropyl Methyl Cellulose(HPMC) E5 LV by Co-Grinding Method

Telmisartan (TMS), an antihypertensive drug, is classified as class II according to Biopharmaceutical Classification System (BCS) with low solubility and high permeability. The purpose of this study was to prepare and characterize solid dispersion of TMS with hidroxypropyl methyl cellulose (HPMC) E5...

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Bibliographic Details
Published in:Oriental journal of chemistry 2017-01, Vol.33 (2), p.873-878
Main Authors: Zaini, Erizal, Fitriani, Lili, Effendy, Sanezea, Noviza, Deni, Halim, Auzal
Format: Article
Language:English
Subjects:
Aluminum
Cellulose
Distilled water
Fourier transforms
Grinding
Particle size
Polymers
Scanning electron microscopy
Solubility
Spectrophotometry
Spectrum analysis
X ray powder diffraction
X-ray diffraction
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Summary:Telmisartan (TMS), an antihypertensive drug, is classified as class II according to Biopharmaceutical Classification System (BCS) with low solubility and high permeability. The purpose of this study was to prepare and characterize solid dispersion of TMS with hidroxypropyl methyl cellulose (HPMC) E5 LV to increase the solubility. Solid dispersion was prepared in three different ratio TMS:HPMC 2:1, 1:1, and 1:2 (w/w) by co-grinding method for 60 minutes. Solubility test was conducted in distilled water for 72 hours and the amount of TMS was determined by spectrophotometry UV. Result of Powder X-Ray Diffraction (PXRD) showed a decrease in intensity of TMS in accordance with the amount of HPMC E5 LV in solid dispersion. Fourier Transform Infra-Red (FT-IR) Spectra showed no significant shift of wavelength. Scanning Electron Microscopy (SEM) result presented the crystalline form of TMS, while both physical mixture and solid dispersion at different ratio showed TMS stick on the surface of HPMC E5 LV. Thermogram of Differential Scanning Calorimetry (DSC) showed an incline of endotherm peak as the ratio HPMC E5 LV increased. The solubility result of intact TMS was 0.49±0.03µg/mL, while the physical mixture and solid dispersion 2:1, 1;1 and 1:2 were 1.87±0.18 µg/mL, 5.36± 0.48 µg/mL, 7.24±1.73 µg/mL, and 14.89±1.49 µg/mL, respectively. In conclusion, solid dispersion of telmisartan-HPMC E5 LV enhanced the solubility of TMS.
ISSN:0970-020X
2231-5039
DOI:10.13005/ojc/330236